Method of reducing weight in mammals

ABSTRACT

Described is a method of decreasing the weight in mammals to a desired amount comprising the steps of ingesting an effective weight reducing amount of a cholestyramine for a desired period of time to achieve a desired weight reduction. Compositions useful for reducing weight in patients contain cholestyramine, bran and optionally, artificial sweeteners and flavors.

TECHNICAL FIELD

The invention is concerned with weight reduction in mammals utilizingion exchange resins.

BACKGROUND ART

A number of references have discussed cholestyramine for varioustherapeutic purposes. U.S. Pat. No. 4,902,501 teaches the use of apharmaceutical composition for oral usage endowed with sequesteringactivity for the biliary acids containing cholestyramine as its activeprinciple further containing at least one anti-microbial agent, onesuspending agent and one coating agent.

U.S. Pat. No. 4,797,288 teaches a drug delivery system designed to bechewed or swallowed comprising cholestyramine, a hydrophobic matrixcontaining an emulsifier and an edible material, a glyceride and acoating material effective to delay hydration until ingested. Thecoating material forms a protective barrier effective to prevent theunpleasant taste perception for the cholestyramine material.

U.S. Pat. No. 4,790,991 teaches an ingestible aggregate containing adietary fiber and a drug that is an anti-cholesterol agent such ascholestyramine.

European patent application No. 332,600 teaches a combination ofcholestyramine and sorbic acid. European patent application 320,519teaches the use of corn syrup or sucrose syrup to assist in eliminatingthe fishy odor of cholestyramine.

U.S. Pat. No. 4,837,255 teaches the use of an improved taste whenaspartame is used as a sweetener.

U.S. Pat. No. 4,759,923 teaches the use of a resin such ascholestyramine as being incorporated in beverages.

Chewable delivery systems for cholestyramine are taught in U.S. Pat. No.4,778,676.

None of the references teach a method of decreasing the weight inmammals by the use of an effective weight reducing amount ofcholestyramine, particularly when combined with bulking agents and/orartificial sweetening agents and flavors.

SUMMARY OF THE INVENTION

Described is a method of decreasing the weight in mammals to a desiredamount comprising the steps of ingesting an effective weight reducingamount of a cholestyramine or a pharmaceutically acceptable salt ormixture thereof for a desired period of time to achieve a desired weightreduction. Compositions useful for reducing weight in patients containcholestyramine, bran, and optionally, artificial sweeteners and flavors.

DESCRIPTION OF PREFERRED EMBODIMENTS

The need for man to achieve desirable weight levels can be affected byutilizing appropriate weight reduction compositions. It has been foundthat the use of cholestyramine as a weight reducing agent in mammals isan effective material. The program for effecting the weight reduction isto utilize a cholestyramine or a pharmaceutically acceptable salt ormixture thereof, preferably in conjunction with palatable materials fora fixed period of time or to achieve the desired weight reduction.

The most preferred cholestyramine is Questran brand (trademark of MeadJohnson for a synthetic anion exchange polymer in which quaternaryammonium groups are attached to a copolymer of styrene and divinylbenzene). The main constituent of Questran is polystyrene trimethylbenzylammonium as Cl anion. Particle size ranges from 50-100 U.S. mesh.

A program that has achieved measurable success is to preparecompositions as described below:

4 grams (1 1/2 measured teaspoons) of powdered wheat bran (0 calories);

4 grams of anhydrous cholestyramine (0 calories);

2 grams (2 packets of) Equal brand of Nutrasweet artificial sweetener (4calories per packet =8 calories);

1 packet of Equal =0.035 gm. (3% of packet by weight) of aspartame plusdextrose and maltodextrin powder as a bulking agent; 0.0965 gm. (96.5%of packet by weight) of powder total added to produce 1 gram/packetincluding bulking agent powder and aspartame;

0.5 grams (1/9 pkg.)--(2/8 calories) of Kool-aid® brand powder drink mixwithout sugar;

2 cups (520 grams) of cold water and crushed ice mixed; or

1/2 pkg. of strawberry flavored Alba® powdered drink mix (35 caloriesand 10 grams);

2 cups of 2% low-fat milk (approximately 125 calories/cup and 555grams);

One or the other of the above two drinks is stirred frequently whilebeing ingested and a drink is taken at least two times a day (threedoses) if one large meal is eaten (either 2 doses just before the mealor 1 dose just before and 1 dose just after or 2 doses just after themeal) and up to three times a day (maximum of five doses per day) ifneeded to allay hunger and/or if two large meals per day are taken.

The most preferred composition utilizing cholestyramine is as follows,with (A) denoting Kool-Aid® brand (unsweetened) and (B) denoting Alba®brand (powdered strawberry shake mix) +2% low-fat milk solids:

    ______________________________________                                                   Preferred     Most Preferred                                                  Range         Ranges                                               Ingredient (In Grams)    (% By Weight)                                        ______________________________________                                        Cholestyramine                                                                           1 to 4        (A) 1/545 × 100% to                                       (0.18% to 0.78%)                                                                              4/534 × 100%                                            (0.17% to 0.70%)                                                                            (B) 1/578 × 100% to                                                       4/568 × 100%                                 Sweetening Agent                                                                         Effective amount,                                                                           (A) 0.07/545 × 100% to                                    e.g. 0.07 (0.013%)                                                            (0.013%)      (B) 0.07/534 × 100%                            Fiber      1 to 8        (A) 1/545 × 100% to                                       (0.18% to 1.50%)                                                                              1/545 × 100%                                            (0.17% to 1.41%)                                                                            (B) 1/578 × 100% to                                                       8/568 × 100%                                 Bulking Agent                                                                            Effective amount,                                                                           (A) 1.93/545 × 100% to                                    e.g. 1.93       1/93/534 × 100%                                         (0.35% to 0.36%)                                                              (0.33% to 0.34%)                                                                            (B) 1.93/578 × 100% to                                                    1.93/568 × 100%                              Carrier    Effective amount,                                                                           (A) 0.2/545 × 100% to                                     e.g. 0.2 to 1.0                                                                               1.0/534 × 100%                                          (0.04% to 0.19%)                                                              67.0          (B) 67/578 × 100% to                                      (12.0% to 12.0%)                                                                              67/568 ×  100%                               Water      530           (A) 530/545 × 100% to                                     (97.24% to 99.25%)                                                                            530/534 × 100%                                          490-497       (B) 497/578 × 100% to                                     (85.99% to 87.5%)                                                                             497/568 × 100%                               ______________________________________                                        Total of all ingredients:                                                     (A) = 534 grams to 545 grams                                                  (B) = 568 grams to 578 grams                                                  Carrier + Water (A) = 530 grams to 531 grams                                  Carrier + Water (B) = 564 grams                                               ______________________________________                                    

While applicant does not wish to be bound by any theory, it is believedthat the use of cholestyramine as a weight reduction agent in mammals,such as humans, is that the patient is satisfied with food sooner. Onefeels full due to the ingestion of the fluid containing thecholestyramine, and therefore, one would eat slowly and ingest a smallerquantity of food. Secondly, it is believed that the use ofcholestyramine inhibits fat from foods from being absorbed. Therefore,there is a partial fat malabsorption. In addition, there is a sedativeeffect, namely that the patient has been found to sleep more soundly dueto the utilization of cholestyramine and this improved sleep reduceshunger as well as reducing total food intake.

Finally, the prevention of bile acid resorption creates a metabolicinefficiency whereby the body utilizes energy to replace some of thecholesterol lost to bile acid binding (failed resorption of bile acids),i.e., the energy required for synthesis of a portion of the cholesterollost to bile acid binding effect. The calories required to resynthesizea portion of those cholesterol molecules lost to bile acid binding wouldbe like the calories which are used up when one exercises vigorously incalculating calorie balance and expected weight change.

The period of time that one wishes to utilize cholestyramine containingmaterials in a weight reduction program is dependent upon the amount ofweight reduction that is desired. Generally, the regimen for takingcholestyramine containing materials is on a daily basis. The length oftime would be minimally one week with longer periods of six months to ayear depending upon the need for weight reduction.

Having described the invention above, listed below are preferredembodiments wherein all parts are parts by weight and all temperaturesare degrees Centigrade unless otherwise indicated.

EXAMPLE

Utilizing the program outlined above and the cholestyramine containingcompositions, several patients were placed on the cholestyramine regimenas follows.

Patient number one is a male caucasian approximately 50 years in age.The regimen was followed for approximately 6 months where the initialweight was 268 pounds and after the 6 month period, the weight of theindividual was 218 pounds.

A second patient was a caucasian female 20 years in age which utilizedthe regimen outlined above for two weeks. The initial weight was 270pounds and the final weight was 255 pounds with a weight reduction ofapproximately 15 pounds.

A third patient was a 13 year old female caucasian. The regimen followedabove resulted in a loss of 22 pounds over a three week period of time;the initial weight was 205 pounds and the final weight was 183 pounds.

While the forms of the invention herein disclosed constitute presentlypreferred embodiments, many others are possible. It is not intendedherein to mention all of the possible equivalent forms or ramificationsof the invention. It is understood that the terms used herein are merelydescriptive rather than limiting, and that various changes may be madewithout departing from the spirit or scope of the invention.

For example, the following drugs may be used in conjunction with theabove program, e.g., Chronulac, trademark of G.D. Searle for lactulose,Lorelco, trademark of Dow for probucol, and the like.

What is claimed is:
 1. A method of reducing weight in mammals to adesired amount comprising orally administering thereto an effectiveweight reducing amount of a cholestyramine or a pharmaceuticallyacceptable salt or mixture thereof containing composition for a desiredperiod of time to achieve a desired weight reduction.
 2. The method ofclaim 1 wherein the cholestyramine containing composition includes abulking agent.
 3. The method of claim 1 wherein the cholestyraminecontaining composition includes an artificial sweetening agent.
 4. Themethod of claim 1 wherein the composition containing cholestyraminecomprising the following materials:

    ______________________________________                                                       Weight Range                                                   Ingredient     (In Grams)                                                     ______________________________________                                        Cholestyramine 1 to 4                                                         Sweetening Agent                                                                             Effective Amount                                               Fiber          1 to 8                                                         Bulking Agent  Effective Amount                                               Carrier        0.2 to 6.7                                                     Water          490-530                                                        ______________________________________                                    


5. The method of claim 1 wherein the cholestyramine composition isutilized for a minimum of one week.